|本期目录/Table of Contents|

[1]崔佳丽,刘红斌,赵高琼,等.ZY2气雾剂小型猪在体透皮药代动力学研究[J].宁夏医科大学学报,2019,(06):546-550.[doi:10.16050/j.cnki.issn1674-6309.2019.06.002]
 CUI Jiali,LIU Hongbin,ZHAO Gaoqiong,et al.Study on the Transdermal Delivery Pharmacokinetic of ZY2 Aerosol in Minipigs[J].Ningxia Medical University,2019,(06):546-550.[doi:10.16050/j.cnki.issn1674-6309.2019.06.002]
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ZY2气雾剂小型猪在体透皮药代动力学研究(PDF)
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《宁夏医科大学学报》[ISSN:1005-8486/CN:64-1029/R]

卷:
期数:
2019年06期
页码:
546-550
栏目:
论著
出版日期:
2019-06-30

文章信息/Info

Title:
Study on the Transdermal Delivery Pharmacokinetic of ZY2 Aerosol in Minipigs
文章编号:
1674-6309(2019)06-0546-05
作者:
崔佳丽123 刘红斌123 赵高琼123 彭 卫123 张培培123 周艺佳123 苏 敏123 王京昆123
(1. 云南省药物研究所,昆明 650111; 2. 云南白药集团创新研发中心,昆明 650111; 3. 云南省中药和民族药新药创制企业重点实验室,昆明 650111)
Author(s):
CUI Jiali123 LIU Hongbin123 ZHAO Gaoqiong123 PENG Wei123 ZHANG Peipei123 ZHOU Yijia123 SU Min123 WANG Jingkun123
(1. Yunnan Institute of Materia Medica,Kunming 650111,China; 2. Yunnan Baiyao Group Innovation and R&D Center,Kunming 650111,China; 3. Yunnan Province Company Key Laboratory for TCM and Ethnic Drug of New Drug Creation,Kunming 650111,China)
关键词:
藜芦胺LC-MS/MS气雾剂小型猪药代动力学
Keywords:
veratramineHPLC-MS/MSaerosolminipigpharmacokinetic
分类号:
R969.1;R917;R965.3
DOI:
10.16050/j.cnki.issn1674-6309.2019.06.002
文献标志码:
A
摘要:
目的 建立一种小型猪血浆藜芦胺的检测方法,研究ZY2气雾剂在不同给药面积、给药量下,检测目标物藜芦胺在小型猪体内的暴露量-给药面积-剂量关系。方法 选用健康普通级巴马小型猪,采用自身交叉实验设计,间隔一周后自身交叉给药,分别给予气雾剂50喷(给药面积10cm×20cm)、100喷(给药面积16cm×25 cm)。 于给药前(0h)和给药完成后0.25、0.5、1.0、2.0、4.0、8.0、11.5、12.0、12.5和24h,眼底静脉窦采血,采用HPLC-MS/MS法检测血浆样品中藜芦胺浓度。结果 1号雌性小型猪进行第一批试验后,仅在12h就检测到藜芦胺,浓度为0.0139ng·mL-1;第二批试验在0.5、1.0和4.0h检测到藜芦胺,1.0h时浓度最高达0.0583ng·mL-1。2号雄性小型猪进行第一批试验后,仅在0.5、1.0、2.0、11.0、11.5和12.0h检测到藜芦胺,0.5h浓度最高达0.676 ng·mL-1;第二批试验后,仅在0.5、4.0、11.0、11.5和12.0 h能检测到藜芦胺,4.0 h浓度最高达0.272 ng·mL-1。结论 建立了一种灵敏、准确、稳定的HPLC-MS/MS测定小型猪血浆中藜芦胺的方法。小型猪自身交叉试验所测得到的藜芦胺血药浓度均极低,故不能有效评估ZY2气雾剂中藜芦胺在小型猪体内的暴露量,进而无法准确有效评估其暴露量-给药面积-剂量的关系。
Abstract:
Objective To establish a method for the determination of veratramine in plasma of minipigs, and to study the relationship between the drug delivery areas,dose and exposure of veratramine in minipigs under different drug delivery areas and doses of ZY2 aerosol. Methods The healthy normal grade BAMA minipigs were designed by self-cross experiment,and they were crossly administrated after one week. Minipigs were administrated with 50 sprays(depilation area of 10cm×20cm) or 100 sprays(depilation area of 16cm×25cm) of aerosol to the back. Blood samples were collected from fundus venous sinuses before dose(0 h)and at 0.25, 0.5,1.0,2.0,4.0,8.0,11.5,12.0,12.5 and 24h respectively after dose. The concentration of veratramine in plasma samples was determined by HPLC-MS/MS. Results Veratramine of No.1 female minipig was detected with the concentration of 0.0139 ng·mL-1 at 12h in the first test batch. Veratramine was only detected at 0.5, 1.0 and 4.0 h in the second test batch, and the highest concentration was 0.0583 ng·mL-1 at 1.0h. Veratramine of No.2 male minipigs was detected at 0.5,1.0,2.0,11.0,11.5 and 12.0 h in the first test batch,and the highest concentration was 0.676 ng·mL-1 at 0.5 h,veratramine was detected at 0.5,4.0,11.0,11.5,and 12.0 h in the second test batch,and the highest concentration was 0.272ng·mL-1 at 4.0h. Conclusion A sensitive, accurate and stable HPLC-MS/MS method for the determination of veratramine in plasma of minipigs was established. The blood concentration of veratramine in minipigs is extremely low by the self-cross tests,so the exposure amount of veratramine in ZY2 aerosol in minipigs cannot be effectively evaluated, and thus the relationship between exposure amount,the dosage area and dose cannot be accurately and effectively evaluated.

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备注/Memo

备注/Memo:
收稿日期:2019-01-02
基金项目:云南省科技创新平台建设计划—科研院所技术开发专项(2016DC030)
作者简介:崔佳丽(1987-),女,工程师,硕士,研究方向:药物代谢、药物安全性评价工作。E-mail:cuijiali19870626@126.com
通信作者:王京昆,正高级工程师,研究方向:药物代谢、药物安全性评价工作。E-mail:3424045368@qq.com
更新日期/Last Update: 2019-06-30